Azaflavones compared to flavones as ligands to the benzodiazepine binding site of brain GABA(A) receptors.
Författare
Summary, in English
A series of azaflavone derivatives and analogues were prepared and evaluated for their affinity to the benzodiazepine binding site of the GABA(A) receptor, and compared to their flavone counterparts. Three of the compounds, the azaflavones 9 and 12 as well as the new flavone 13, were also assayed on GABA(A) receptor subtypes (alpha(1)beta(3)gamma(2s), alpha(2)beta(3)gamma(2s), alpha(4)beta(3)gamma(2s) and alpha(5)beta(3)gamma(2s)), displaying nanomolar affinities as well as selectivity for alpha1- versus alpha2- and alpha3-containing receptors by a factor of between 14 and 26.
Avdelning/ar
Publiceringsår
2008
Språk
Engelska
Sidor
5713-5716
Publikation/Tidskrift/Serie
Bioorganic & Medicinal Chemistry Letters
Volym
18
Issue
21
Dokumenttyp
Artikel i tidskrift
Förlag
Elsevier
Ämne
- Organic Chemistry
Status
Published
ISBN/ISSN/Övrigt
- ISSN: 0960-894X